Gobec Stanislav, Sova Matej, Kristan Katja, Rizner Tea Lanisnik
Faculty of Pharmacy, University of Ljubljana, Askerceva 7, 1000 Ljubljana, Slovenia.
Bioorg Med Chem Lett. 2004 Aug 2;14(15):3933-6. doi: 10.1016/j.bmcl.2004.05.069.
We present the synthesis of a new family of nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase, designed from flavones and chalcones. Their inhibitory potential was screened on 17beta-hydroxysteroid dehydrogenase from the fungus Cochliobolus lunatus (17beta-HSDcl), a model enzyme of the short-chain dehydrogenase/reductase superfamily. In a series of cinnamates and related coumarin-3-carboxylates, a number of compounds proved to be potent inhibitors of both the oxidative and reductive reactions catalyzed by 17beta-HSDcl, with IC(50) values in the low micromolar range.
我们展示了一类新的17β-羟基类固醇脱氢酶非甾体抑制剂的合成，该抑制剂是基于黄酮和查耳酮设计的。它们的抑制潜力在来自新月弯孢菌（17β-HSDcl）的17β-羟基类固醇脱氢酶上进行了筛选，该酶是短链脱氢酶/还原酶超家族的一种模型酶。在一系列肉桂酸酯和相关的香豆素-3-羧酸酯中，许多化合物被证明是17β-HSDcl催化的氧化和还原反应的有效抑制剂，其半数抑制浓度（IC50）值处于低微摩尔范围。
